59868-48-3

Upstream product

• 5900-58-3 2-amino-4-chloro-benzoic acid methyl ester 
• 144-55-8 sodium hydrogencarbonate 
• 1490-25-1 succinic acid monomethylester chloride 

Downstream Products

• 87379-41-7 8-chloro-1,3,4,5-tetrahydro-2H-1-benzazepin-2,5-dione 
• 1350816-20-4 9-chloro-2-({3-[3-(dimethylamino)propyl]-2-methoxyphenyl}amino)-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepine-6-thione 
• 1350816-18-0 9-chloro-2-{[3-[3-(dimethylamino)propyl]-4-(trifluoromethyl)phenyl]amino}-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepine-6-thione 
• 1350816-17-9 9-chloro-2-({3-[3-(dimethylamino)propyl]-4-methoxyphenyl}amino)-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepine-6-thione hydrochloride 
• 1350816-15-7 9-chloro-2-({3-[3-(dimethylamino)propyl]-4-fluorophenyl}amino)-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepine-6-thione 
• 1350816-11-3 9-chloro-2-({5-[3-(dimethylamino)propyl]-2-isopropylphenyl}amino)-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepine-6-thione 
• 1350816-09-9 9-chloro-2-(5-(3-(dimethylamino)propyl)-2-(trifluoromethyl)phenylamino)-5H-benzo[b]pyrimido[4,5-d]azepine-6(7H)-thione 
• 1350816-07-7 9-chloro-2-{[5-[3-(dimethylamino)propyl]-2-(trifluoromethoxy)phenyl]amino}-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepine-6-thione 
• 1350816-04-4 9-chloro-2-({2-chloro-5-[3-(dimethylamino)propyl]phenyl}amino)-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepine-6-thione 
• 1350816-02-2 9-chloro-2-(5-(3-(dimethylamino)propyl)-2-methylphenylamino)-5H-benzo[b]pyrimido[4,5-d]azepine-6(7H)-thione 
• 1350816-00-0 9-chloro-2-(3-morpholinophenylamino)-5H-benzo[b]pyrimido[4,5-d]azepin-6(7H)-one hydrochloride 
• 1350815-99-4 9-chloro-2-({3-[2-(dimethylamino)ethoxy]phenyl}amino)-5,7-dihydro-6H-pyrimido[5,4-d][1]benzazepin-6-one 
• 1350815-97-2 9-chloro-2-(3-((4-methylpiperazin-1-yl)methyl)phenylamino)-5H-benzo[b]pyrimido[4,5-d]azepin-6(7H)-one 
• 1350815-96-1 2-(3-(3-aminopropyl)phenylamino)-9-chloro-5H-benzo[b]pyrimido[4,5-d]azepin-6(7H)-one 

Relevant academic research and scientific papers

5-Substituted 3-chlorokenpaullone derivatives are potent inhibitors of Trypanosoma brucei bloodstream forms

Trypanothione synthetase is an essential enzyme for kinetoplastid parasites which cause highly disabling and fatal diseases in humans and animals. Inspired by the observation that N(5)-substituted paullones inhibit the trypanothione synthetase from the related parasite Leishmania infantum, we designed and synthesized a series of new derivatives. Although none of the new compounds displayed strong inhibition of Trypanosoma brucei trypanothione synthetase, several of them caused a remarkable growth inhibition of cultivated Trypanosoma brucei bloodstream forms. The most potent congener 3a showed antitrypanosomal activity in double digit nanomolar concentrations and a selectivity index of three orders of magnitude versus murine macrophage cells.

Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of polo-like kinase 1 (MLN0905)

This article describes the discovery of a series of potent inhibitors of Polo-like kinase 1 (PLK1). Optimization of this benzolactam-derived chemical series produced an orally bioavailable inhibitor of PLK1 (12c, MLN0905). In vivo pharmacokinetic-pharmacodynamic experiments demonstrated prolonged mitotic arrest after oral administration of 12c to tumor bearing nude mice. A subsequent efficacy study in nude mice achieved tumor growth inhibition or regression in a human colon tumor (HT29) xenograft model.

4-Carbamoyl-1-benzazepines as antiinflammatory agents

4-Arylcarbamoyl-2,3,4,5-tetrahydro-1-benzazepine-2,5-diones, e.g. those of the fromula SPC1 R = h, alkyl or aralkyl Ar = iso- or heterocyclic aryl R',r" = h, alkyl, alkanoyl, alkoxy, halogen or CF3 alkali metal or acid addition salts thereof are antiinflammatory agents.

4-Carbamoyl-1-benzazepines

4-Arylcarbamoyl-2,3,4,5-tetrahydro-1-benzazepine-2,5-diones, e.g. those of the formula SPC1 R = h, alkyl or aralkyl Ar = iso- or heterocyclic aryl R',r" = h, alkyl, alkanoyl, alkoxy, halogen or CF3 alkali metal or acid addition salts thereof are antiinflammatory agents.